CN102512656B - Quinapril hydrochloride medicinal composition - Google Patents
Quinapril hydrochloride medicinal composition Download PDFInfo
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- CN102512656B CN102512656B CN201110444527XA CN201110444527A CN102512656B CN 102512656 B CN102512656 B CN 102512656B CN 201110444527X A CN201110444527X A CN 201110444527XA CN 201110444527 A CN201110444527 A CN 201110444527A CN 102512656 B CN102512656 B CN 102512656B
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- quinapril hydrochloride
- pharmaceutical composition
- lactose
- quinapril
- pregelatinized starch
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Abstract
The invention discloses a quinapril hydrochloride medicinal composition, which is characterized by comprising the following components in percentage by weight: 5 to 20 percent of quinapril hydrochloride, 20 to 70 percent of lactose, 10 to 30 percent of pregelatinized starch, 5 to 20 percent of crospovidone, and 0.5 to 2 percent of silicon dioxide. The quinapril hydrochloride medicinal composition with high stability can promote product yield increase, cost reduction, industrialization and good clinic use and has obvious advantages.
Description
Technical field
The present invention relates to the medicine in field of medicaments, especially relate to quinapril hydrochloride pharmaceutical composition of a kind of sustainable release and preparation method thereof.
Background technology
Quinapril hydrochloride is without dredging base, long-acting, oral Angiotensin-Converting (ACE) inhibitor.After oral, be hydrolyzed into the activated two acid type compounds of tool at liver, be quinaprilat, can suppress ACE, the prevention angiotensin i-converting is Angiotensin II, thereby the vasoconstrictor effects that Angiotensin II mediates is obviously weakened, reduce the vascular resistance of tremulous pulse; Also suppress simultaneously the synthetic of aldosterone, the water that the minimizing aldosterone produces and the retention of sodium, further descend blood pressure.Thereby be a kind of safe, efficient antihypertensive drugs.Being applicable to the routine medication effect is unsatisfied with or more hypertension and the congestive heart failure person of untoward reaction.Suitable with enalapril in the former this product curative effect, be better than captopril; After latter's prolonged application, this product effect does not subtract, and can obviously improve symptom and increase motor capacity.
Common name: quinapril hydrochloride;
English name: Quinapril hydrochloride;
CAS：82586-55-8；
Chemical name: S-2[N-[(S)-1-ethoxycarbonyl-3-phenylpropyl]-the L-alanyl]-1,2,3,4-tetrahydrochysene-3-isoquinolin hydrochlorate;
Chemical structural formula:
Molecular formula: C
25H
30N
2O
5HCl;
Molecular weight: 438.52;
Outward appearance: white or off-white color crystalline powder.
Patent, have no the related preparations patent report both at home and abroad.
In order to meet the doctor, the clinical application demand, increase its preparation type and specification, and inventor's process studies for a long period of time, quinapril hydrochloride pharmaceutical composition prepared by Optimization Technology, and good stability, dissolution rate is fast, and bioavailability is high.Not only successfully solved the problem of the poor stability of quinapril hydrochloride, improved bioavailability, reduced production costs, easy to implement, can realize industrialization, remarkable in economical benefits.
Summary of the invention
The first purpose of the present invention is to provide a kind of quinapril hydrochloride pharmaceutical composition, this quinapril hydrochloride pharmaceutical composition good stability, and dissolution rate is fast, bioavailability is high, to improving product yield, reduces costs, realize industrialization, better be applied to clinically, have more obvious advantage.
The second purpose of the present invention is to provide the preparation method of quinapril hydrochloride pharmaceutical composition of the present invention, and the method is simple, prepared quinapril hydrochloride pharmaceutical composition good stability.
The inventor, through a large amount of tests, is surprised to find at quinapril hydrochloride drug regimen species, gives lactose and the starch of proper proportion, adds other adjuvants, also can meet the preparation requirement.
Pharmaceutical composition provided by the present invention is comprised of following composition and percentage by weight: 5%-20% quinapril hydrochloride, the silicon dioxide of 20%-70% lactose, 10-30% pregelatinized Starch, 5%-20% polyvinylpolypyrrolidone, 0.5%-2% weight.
Be preferably, every 1000 described quinapril hydrochloride pharmaceutical compositions, its formula consists of:
Quinapril hydrochloride 10%
Lactose 65%
Pregelatinized Starch 16%
Polyvinylpolypyrrolidone 8%
Silica 1 %
Purified water is appropriate.
Quinapril hydrochloride pharmaceutical composition of the present invention adopts following method to prepare:
Quinapril hydrochloride, lactose, pregelatinized Starch, polyvinylpolypyrrolidone are placed in and tell mixer, mix 3-5 minute, make mix homogeneously; In the material of above-mentioned mix homogeneously, add purified water appropriate, make the soft material of suitable hardness; Adopt 20 eye mesh screens to make the granule that granularity is suitable soft material; Airpillow-dry to pellet moisture is less than 5% under 60 ± 5 ℃ of conditions; Granule is taken out, add silicon dioxide to mix 20 minutes mix homogeneously; Intermediate detects, detection level, and the indexs such as moisture, according to the heavy scope of cubage sheet; Tabletting, obtain.
The inventor finds through a large amount of experimental study, when the quinapril hydrochloride pharmaceutical composition is above-mentioned formula, and described pharmaceutical composition the best in quality, stability is best.
Another aspect of the present invention provides the preparation method of quinapril hydrochloride pharmaceutical composition of the present invention, and the method is simple, prepared quinapril hydrochloride pharmaceutical composition good stability, and bioavailability is high.
The quinapril hydrochloride pharmaceutical composition made according to the inventive method, through industrial amplification production and study on the stability, proves that product is stable, through pharmacology, toxicological test, to human body without injury.
Below by test data, beneficial effect of the present invention is described.
With the product of the embodiment of the present invention 1, investigate indices as follows:
Embodiment 1 accelerated test result
Upper table demonstration, the sample quality of the embodiment of the present invention 1 is stable, and stripping is fast, and bioavailability is high, and impurity changes little, and steady quality is reliable.
The invention has the advantages that, overcome problem in prior art, product can be maintained a long-term stability.
The present invention has following advantage:
1) new quinapril hydrochloride compositions provided by the present invention has thoroughly solved the stability problem of quinapril hydrochloride.
2) quinapril hydrochloride pharmaceutical composition provided by the present invention is for the market risk of the yield that improves this product, reduction product, and better being applied to clinical treatment has very large help.
3) new quinapril hydrochloride compositions provided by the present invention, through industrialized great production and study on the stability, proves constant product quality, through pharmacology, toxicological test, to human body without injury.
4) preparation method of new quinapril hydrochloride compositions provided by the present invention, the method is simple, prepared quinapril hydrochloride pharmaceutical composition good stability, bioavailability is high.
The specific embodiment
Below in conjunction with embodiment, the present invention is described in further detail
Embodiment 1
Every 1000 described quinapril hydrochloride pharmaceutical compositions, its formula consists of:
Quinapril hydrochloride 10%
Lactose 65%
Pregelatinized Starch 16%
Polyvinylpolypyrrolidone 8%
Silica 1 %
Purified water is appropriate.
Preparation technology:
Quinapril hydrochloride, lactose, pregelatinized Starch, polyvinylpolypyrrolidone are placed in and tell mixer, mix 3-5 minute, make mix homogeneously; In the material of above-mentioned mix homogeneously, add purified water appropriate, make the soft material of suitable hardness; Adopt 20 eye mesh screens to make the granule that granularity is suitable soft material; Airpillow-dry to pellet moisture is less than 5% under 60 ± 5 ℃ of conditions; Granule is taken out, add silicon dioxide to mix 20 minutes mix homogeneously; Intermediate detects, detection level, and the indexs such as moisture, according to the heavy scope of cubage sheet; Tabletting, obtain.
Embodiment 2
Every 1000 described quinapril hydrochloride pharmaceutical compositions, its formula consists of:
Quinapril hydrochloride 10g
Lactose 65g
Pregelatinized Starch 16g
Polyvinylpolypyrrolidone 8g
Silica 1 g
Purified water is appropriate.
Preparation technology: with embodiment 1.
Embodiment 3
Every 1000 described quinapril hydrochloride pharmaceutical compositions, its formula consists of:
Quinapril hydrochloride 5%
Lactose 70%
Pregelatinized Starch 14%
Polyvinylpolypyrrolidone 10%
Silica 1 %
Purified water is appropriate.
Preparation technology: with embodiment 1.
Embodiment 4
Every 1000 described quinapril hydrochloride pharmaceutical compositions, its formula consists of:
Quinapril hydrochloride 10g
Lactose 120g
Pregelatinized Starch 28g
Polyvinylpolypyrrolidone 20g
Silicon dioxide 2g
Purified water is appropriate.
Preparation technology: with embodiment 1.
Test example 1
This test example is to investigate the stability of quinapril hydrochloride compositions provided by the present invention.
The accelerated test of quinapril hydrochloride pharmaceutical composition
Method according to the embodiment of the present invention 1 prepares three batches of quinapril hydrochloride pharmaceutical compositions (lot number is respectively SR1005101, SR1005102, SR1005103) according to commercially available back, at 40 ℃ ± 2 ℃, the condition of RH75% ± 5% was placed 6 months, during this time respectively at sampling in the 1st, 2,3,6 months, according to the stability inspection item, detect, and compare with 0 day data.
Above conclusion (of pressure testing) can be found out: this product is placed 6 months every detection indexs and with 0 month, is compared no significant difference, good stability under long term test and accelerated test condition.
Claims (1)
1. a quinapril hydrochloride pharmaceutical composition, is characterized in that, its described quinapril hydrochloride pharmaceutical composition, and every 1000 its formulas consist of:
Quinapril hydrochloride 10g
Lactose 65g
Pregelatinized Starch 16g
Polyvinylpolypyrrolidone 8g
Silica 1 g
Purified water is appropriate
The preparation method of quinapril hydrochloride pharmaceutical composition comprises the steps:
Quinapril hydrochloride, lactose, pregelatinized Starch, polyvinylpolypyrrolidone are placed in to high-speed mixer, mix 3-5 minute, make mix homogeneously; In the material of above-mentioned mix homogeneously, add purified water appropriate, make the soft material of suitable hardness; Adopt 20 eye mesh screens to make the granule that granularity is suitable soft material; Airpillow-dry to pellet moisture is less than 5% under 60 ± 5 ℃ of conditions; Granule is taken out, add silicon dioxide to mix 20 minutes mix homogeneously; Intermediate detects, detection level, and moisture content index, according to the heavy scope of cubage sheet; Tabletting, obtain.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201110444527XA CN102512656B (en) | 2011-12-27 | 2011-12-27 | Quinapril hydrochloride medicinal composition |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201110444527XA CN102512656B (en) | 2011-12-27 | 2011-12-27 | Quinapril hydrochloride medicinal composition |
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| CN102512656A CN102512656A (en) | 2012-06-27 |
| CN102512656B true CN102512656B (en) | 2013-11-27 |
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| CN201110444527XA Active CN102512656B (en) | 2011-12-27 | 2011-12-27 | Quinapril hydrochloride medicinal composition |
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| WO2022184113A1 (en) * | 2021-03-03 | 2022-09-09 | 苏州盛迪亚生物医药有限公司 | Pharmaceutical composition comprising pyridopyrimidine derivative, and preparation method therefor |
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| IL139590A0 (en) * | 1998-06-05 | 2002-02-10 | Warner Lambert Co | Stabilization of compositions containing ace inhibitors using magnesium oxide |
| CN1618426A (en) * | 2003-11-21 | 2005-05-25 | 上海旭东海普药业有限公司 | Medicinal composition contg. katopril, and its prepn. method |
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Effective date of registration: 20140319 Address after: 300250 Taixing apartment, Taixing Road, Tianjin, 14-1-102 Patentee after: Yang Xiaoman Address before: 300250 Taixing apartment, Taixing Road, Hedong District, Tianjin, 14-1-102 Patentee before: Tianjin Songrui Medical Technology Co.,Ltd. |
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Inventor after: Zhang Hao Inventor after: Sun Jingshun Inventor after: Ding Fei Inventor after: Hu Zhengfang Inventor before: Zhang Hao |
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